Vorozole: Difference between revisions

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{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 470631940
| IUPAC_name = 6-[(4-Chlorophenyl)(1,2,4-triazol-1-yl)methyl]-1-methylbenzotriazole
| image = Vorozole.svg


<!--Clinical data-->
| tradename = 
| pregnancy_category = 
| legal_status = 
| routes_of_administration = 


<!--Pharmacokinetic data-->
| bioavailability = Very high
| metabolism = Hepatic
| elimination_half-life = 8 hours
| excretion = 


{{Drugbox|
<!--Identifiers-->
|IUPAC_name = 6-[(4-chlorophenyl)-(1,2,4-triazol-1-yl)methyl]-<br>1-methyl-benzotriazole
| CAS_number_Ref = {{cascite|changed|??}}
| image= Vorozole.svg
| CAS_number = 118949-22-7
| CAS_number=118949-22-7
| ATC_prefix = L02
| ATC_prefix=L02
| ATC_suffix = BG05
| ATC_suffix=BG05  
| PubChem = 6918191
| ATC_supplemental=
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| PubChem=60796
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| DrugBank=
| ChemSpiderID = 5293402
| C = 16 | H = 13 | Cl = 1 | N = 6  
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 1E2S9YXV2A
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D03786
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 224060
 
<!--Chemical data-->
| C=16 | H=13 | Cl=1 | N=6  
| molecular_weight = 324.768 g/mol
| molecular_weight = 324.768 g/mol
| bioavailability=  
| smiles = Clc1ccc(cc1)[C@@H](c2ccc3nnn(c3c2)C)n4ncnc4
| metabolism =  
| InChI = 1/C16H13ClN6/c1-22-15-8-12(4-7-14(15)20-21-22)16(23-10-18-9-19-23)11-2-5-13(17)6-3-11/h2-10,16H,1H3/t16-/m0/s1
| elimination_half-life=
| InChIKey = XLMPPFTZALNBFS-INIZCTEOBI
| excretion = 
| pregnancy_category =
| legal_status =
| routes_of_administration=  
}}
}}
{{SI}}
'''Vorozole''' is an [[aromatase inhibitor]] used as an [[antineoplastic]] agent.


'''Vorozole''' is an [[imidazole]] based [[competitive inhibitor]] of the [[aromatase]] enzyme.  It underwent clinical testing for evaluation for use as an [[antineoplastic]] agent; however it was withdrawn from testing when no difference was detected in the duration of median survival as compared to the progestational agent [[megestrol acetate]] and research instead focused on the other third generation [[aromatase inhibitors]] [[anastrozole]], [[letrozole]] and [[exemestane]].
It is selective.<ref name="pmid9797019">{{cite journal |author=Goss PE |title=Pre-clinical and clinical review of vorozole, a new third generation aromatase inhibitor |journal=Breast Cancer Res. Treat. |volume=Suppl 1 |issue= |pages=S59–65; discussion S73–7 |series=49 |year=1998 |pmid=9797019 |doi= 10.1023/a:1006052923468 |url=http://www.kluweronline.com/art.pdf?issn=0167-6806&volume=49%20Suppl%201&page=S59}}</ref>
==References==
{{Reflist}}
{{Androgenics}}
{{Estrogenics}}


{{Sex hormones}}
[[Category:Aromatase inhibitors]]
[[Category:Aromatase inhibitors]]
[[Category:Endocrinology]]
[[Category:Organochlorides]]
{{WikiDoc Help Menu}}
[[Category:Triazoles]]
{{WikiDoc Sources}}
[[Category:Benzotriazoles]]
 
 
{{antineoplastic-drug-stub}}

Revision as of 15:46, 10 April 2015

Vorozole
Clinical data
ATC code
Pharmacokinetic data
BioavailabilityVery high
MetabolismHepatic
Elimination half-life8 hours
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC16H13ClN6
Molar mass324.768 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Vorozole is an imidazole based competitive inhibitor of the aromatase enzyme. It underwent clinical testing for evaluation for use as an antineoplastic agent; however it was withdrawn from testing when no difference was detected in the duration of median survival as compared to the progestational agent megestrol acetate and research instead focused on the other third generation aromatase inhibitors anastrozole, letrozole and exemestane.

It is selective.[1]

References

  1. Goss PE (1998). "Pre-clinical and clinical review of vorozole, a new third generation aromatase inhibitor" (PDF). Breast Cancer Res. Treat. 49. Suppl 1: S59–65, discussion S73–7. doi:10.1023/a:1006052923468. PMID 9797019.



Template:Antineoplastic-drug-stub